Podophyllotoxin and 4′-demethylepipodophyllotoxin have structures as illustrated on formulas (I) and (II) in FIG. 1; podophyllotoxin and 4′-demethylepipodophyllotoxin are natural active lead compounds with unique anti-tumor activity extracted from podophyllotoxin-type plants (such as Berberidaceae Sinopodophyllum hexandrum, umbrellaleaf, dysosma versipellis etc.), with shortcomings such as strong toxic and side effect and poor bioavailability limiting their clinical application.